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WO2008106186A3 - Activated polyoxazolines and compositions comprising the same - Google Patents

Activated polyoxazolines and compositions comprising the same Download PDF

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Publication number
WO2008106186A3
WO2008106186A3 PCT/US2008/002626 US2008002626W WO2008106186A3 WO 2008106186 A3 WO2008106186 A3 WO 2008106186A3 US 2008002626 W US2008002626 W US 2008002626W WO 2008106186 A3 WO2008106186 A3 WO 2008106186A3
Authority
WO
WIPO (PCT)
Prior art keywords
poz
derivatives
activated
present disclosure
disclosed
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2008/002626
Other languages
French (fr)
Other versions
WO2008106186A2 (en
Inventor
J Milton Harris
Michael David Bentley
Kunsang Yoon
Zhihao Fang
Francesco Maria Veronese
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Serina Therapeutics Inc
Original Assignee
Serina Therapeutics Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Serina Therapeutics Inc filed Critical Serina Therapeutics Inc
Priority to JP2009551999A priority Critical patent/JP5615558B2/en
Priority to CN200880013983A priority patent/CN101686687A/en
Priority to EP08726203A priority patent/EP2134181A4/en
Priority to US12/529,001 priority patent/US7943141B2/en
Priority to KR20097020124A priority patent/KR101508617B1/en
Priority to KR20137028233A priority patent/KR101508621B1/en
Publication of WO2008106186A2 publication Critical patent/WO2008106186A2/en
Publication of WO2008106186A3 publication Critical patent/WO2008106186A3/en
Anticipated expiration legal-status Critical
Priority to US13/961,576 priority patent/US20140011964A1/en
Priority to US14/550,571 priority patent/US20150079658A1/en
Priority to US14/663,863 priority patent/US20150190526A1/en
Priority to US15/453,686 priority patent/US10086084B2/en
Priority to US16/144,358 priority patent/US10864276B2/en
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G73/00—Macromolecular compounds obtained by reactions forming a linkage containing nitrogen with or without oxygen or carbon in the main chain of the macromolecule, not provided for in groups C08G12/00 - C08G71/00
    • C08G73/06—Polycondensates having nitrogen-containing heterocyclic rings in the main chain of the macromolecule
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/74—Synthetic polymeric materials
    • A61K31/785—Polymers containing nitrogen
    • A61K31/787—Polymers containing nitrogen containing heterocyclic rings having nitrogen as a ring hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/44—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members
    • C07D207/444—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5
    • C07D207/448—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide
    • C07D207/452—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having three double bonds between ring members or between ring members and non-ring members having two doubly-bound oxygen atoms directly attached in positions 2 and 5 with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to other ring carbon atoms, e.g. maleimide with hydrocarbon radicals, substituted by hetero atoms, directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/46—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G73/00—Macromolecular compounds obtained by reactions forming a linkage containing nitrogen with or without oxygen or carbon in the main chain of the macromolecule, not provided for in groups C08G12/00 - C08G71/00
    • C08G73/02—Polyamines
    • C08G73/0233—Polyamines derived from (poly)oxazolines, (poly)oxazines or having pendant acyl groups
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08K—Use of inorganic or non-macromolecular organic substances as compounding ingredients
    • C08K5/00—Use of organic ingredients
    • C08K5/16—Nitrogen-containing compounds
    • C08K5/34—Heterocyclic compounds having nitrogen in the ring
    • C08K5/3412—Heterocyclic compounds having nitrogen in the ring having one nitrogen atom in the ring
    • C08K5/3415—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L79/00—Compositions of macromolecular compounds obtained by reactions forming in the main chain of the macromolecule a linkage containing nitrogen with or without oxygen or carbon only, not provided for in groups C08L61/00 - C08L77/00
    • C08L79/02—Polyamines
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L79/00—Compositions of macromolecular compounds obtained by reactions forming in the main chain of the macromolecule a linkage containing nitrogen with or without oxygen or carbon only, not provided for in groups C08L61/00 - C08L77/00
    • C08L79/04—Polycondensates having nitrogen-containing heterocyclic rings in the main chain; Polyhydrazides; Polyamide acids or similar polyimide precursors

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Polyethers (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Macromolecular Compounds Obtained By Forming Nitrogen-Containing Linkages In General (AREA)
  • Pyrrole Compounds (AREA)
  • Solid-Sorbent Or Filter-Aiding Compositions (AREA)

Abstract

The present disclosure provides terminally activated monofunctional POZ derivatives having a range of functional active groups allowing conjugation of the monofunctional POZ derivatives to a variety of target molecules under a wide range of reaction conditions to produce a hydrolytically stable target molecule-POZ conjugate. Furthermore, the present disclosure provides novel methods of synthesis for the disclosed terminally activated monofunctional POZ derivatives and hydrolytically stable target molecule-POZ conjugates created using the disclosed terminally activated monofunctional POZ derivatives.
PCT/US2008/002626 2007-02-28 2008-02-28 Activated polyoxazolines and compositions comprising the same Ceased WO2008106186A2 (en)

Priority Applications (11)

Application Number Priority Date Filing Date Title
JP2009551999A JP5615558B2 (en) 2007-02-28 2008-02-28 Active polyoxazoline and compositions containing the same
CN200880013983A CN101686687A (en) 2007-02-28 2008-02-28 Activated polyoxazolines and compositions containing same
EP08726203A EP2134181A4 (en) 2007-02-28 2008-02-28 ACTIVATED POLYOXAZOLINS AND COMPOSITIONS CONTAINING THEREOF
US12/529,001 US7943141B2 (en) 2007-02-28 2008-02-28 Activated polyoxazolines and compositions comprising the same
KR20097020124A KR101508617B1 (en) 2007-02-28 2008-02-28 Activated polyoxazolines and compositions comprising the same
KR20137028233A KR101508621B1 (en) 2007-02-28 2008-02-28 Activated polyoxazolines and compositions comprising the same
US13/961,576 US20140011964A1 (en) 2007-02-28 2013-08-07 Activated Polyoxazolines and Conjugates and Compositions Comprising the Same
US14/550,571 US20150079658A1 (en) 2007-02-28 2014-11-21 Activated Polyoxazolines and Conjugates and Compositions Comprising the Same
US14/663,863 US20150190526A1 (en) 2007-02-28 2015-03-20 Activated Polyoxazolines and Conjugates and Compositions Comprising the Same
US15/453,686 US10086084B2 (en) 2007-02-28 2017-03-08 Activated polyoxazolines and conjugates and compositions comprising the same
US16/144,358 US10864276B2 (en) 2007-02-28 2018-09-27 Activated polyoxazolines and conjugates and compositions comprising the same

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US89221207P 2007-02-28 2007-02-28
US60/892,212 2007-02-28

Related Child Applications (4)

Application Number Title Priority Date Filing Date
US12/529,001 A-371-Of-International US7943141B2 (en) 2007-02-28 2008-02-28 Activated polyoxazolines and compositions comprising the same
US15529001 A-371-Of-International 2008-02-28
US12529001 A-371-Of-International 2009-08-27
US62226409A Continuation-In-Part 2007-02-28 2009-11-19

Publications (2)

Publication Number Publication Date
WO2008106186A2 WO2008106186A2 (en) 2008-09-04
WO2008106186A3 true WO2008106186A3 (en) 2008-10-23

Family

ID=39721806

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/002626 Ceased WO2008106186A2 (en) 2007-02-28 2008-02-28 Activated polyoxazolines and compositions comprising the same

Country Status (6)

Country Link
US (1) US7943141B2 (en)
EP (1) EP2134181A4 (en)
JP (1) JP5615558B2 (en)
KR (2) KR101508617B1 (en)
CN (2) CN106046370A (en)
WO (1) WO2008106186A2 (en)

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US11622993B2 (en) 2017-08-03 2023-04-11 Synthorx, Inc. Cytokine conjugates for the treatment of autoimmune diseases
US12234271B2 (en) 2019-09-10 2025-02-25 Synthorx, Inc. Il-2 conjugates and methods of use to treat autoimmune diseases
US12319944B2 (en) 2017-07-11 2025-06-03 The Scripps Research Institute Incorporation of unnatural nucleotides and methods thereof

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US8101706B2 (en) 2008-01-11 2012-01-24 Serina Therapeutics, Inc. Multifunctional forms of polyoxazoline copolymers and drug compositions comprising the same
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US20110318322A1 (en) 2009-01-12 2011-12-29 Nektar Therapeutics Conjugates of a Lysosomal Enzyme Moiety and a Water Soluble Polymer
CA2816722C (en) 2010-11-12 2022-03-15 Nektar Therapeutics Conjugates of an il-2 moiety and a polymer
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US10894087B2 (en) 2010-12-22 2021-01-19 Nektar Therapeutics Multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds
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Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12319944B2 (en) 2017-07-11 2025-06-03 The Scripps Research Institute Incorporation of unnatural nucleotides and methods thereof
US11622993B2 (en) 2017-08-03 2023-04-11 Synthorx, Inc. Cytokine conjugates for the treatment of autoimmune diseases
US11701407B2 (en) 2017-08-03 2023-07-18 Synthorx, Inc. Cytokine conjugates for the treatment of proliferative and infectious diseases
US12318431B2 (en) 2017-08-03 2025-06-03 Synthorx, Inc. Cytokine conjugates for the treatment of proliferative and infectious diseases
US12377131B2 (en) 2017-08-03 2025-08-05 Synthorx, Inc. Cytokine conjugates for the treatment of autoimmune diseases
US12234271B2 (en) 2019-09-10 2025-02-25 Synthorx, Inc. Il-2 conjugates and methods of use to treat autoimmune diseases

Also Published As

Publication number Publication date
CN106046370A (en) 2016-10-26
US20100069579A1 (en) 2010-03-18
JP5615558B2 (en) 2014-10-29
WO2008106186A2 (en) 2008-09-04
EP2134181A4 (en) 2011-09-28
KR20130125404A (en) 2013-11-18
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US7943141B2 (en) 2011-05-17
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